Synthesis of 1,2,3,4-Tetrahydroeudistomin U Derivatives and Preliminary In Vitro. Antitumor Evaluation

Abstract

A series of novel 2-substituted 1,2,3,4-tetrahydroeudistomin U derivatives were synthesized by the key Pictet-Spengler cyclization reaction and their in vitro. antitumor activities were evaluated using Pyricularia oryzae. Cavara and Caco-2 cancer cells. Most of the 2-alkyl-1,2,3,4-tetrahydroeudistomin U compounds (19– 23) showed potent inhibitory activities in both of the biological tests. Preliminary structure-activity relationships are also presented.

Keywords:

• Antitumor
• Caco-2 cancer cell
• 1-(indol-3-yl)-1,2,3,4-tetrahydro-β-carboline
• Pyricularia oryzae